P450
Cytochrome P450 are a family of heme-containing monoxygenases catalyzing the metabolism of xenobiotics in the body where P450 enzymes use O2 and two electrons provided by NAD(P)H with the help of redox partner flavoproteins and iron-sulfur proteins to catalyze the monooxygenation of a variety of substrates. Based on how electrons from NAD(P)H are delivered to the catalytic site, P450 enzymes are divided into four classes, including Class I requiring both an FAD-containing reductase and an iron sulfur redoxin, Class II requiring only an FAD/FMN-containg P450 reductase, Class III requiring no electron donor and Class IV requiring electrons directly from NAD(P)H.
Products for P450
- Cat.No. 产品名称 Information
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GC91296
p-Carboxyphenyl Sulfate
一种硫酸化的酚酸。
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GC91226
10-Chloroestra-1,4-diene-3,17-dione
一种雌激素受体α激动剂
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GC91189
Piperonyl Butoxide-d9
一种用于定量苯甲酸对氧乙基的内部标准。
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GC91128
Imazalil-d5 (sulfate)
一种用于量化伊马唑啉的内部标准
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GC90195
Posaconazole-d5
一种用于量化泊沙康唑的内部标准。
- GC69602 Obtusifoliol Obtusifoliol 是一种特异的 CYP51 抑制剂,Obtusifoliol 对布鲁氏锥虫 (TB) 和人 CYP51 的亲和力的 Kd 值分别为 1.2 µM 和 1.4 µM。
- GC68926 TP0472993 CYP4A11/CYP4F2-IN-2 是一种有效和具有口服活性的细胞色素 P450 (CYP) 4A11 和 CYP4F2 的双抑制剂,IC50 值分别分别为 140 nM 和 40 nM。CYP4A11/CYP4F2-IN-2 具有研究肾脏疾病的潜力。
- GC68863 Cholesterol 24-hydroxylase-IN-1 Cholesterol 24-hydroxylase-IN-1 (compound 17) 是一种强效、口服活性和高选择性的胆固醇24-羟化酶 (CH24H or CYP46A1) 抑制剂 (IC50=8.5 nM)。Cholesterol 24-hydroxylase-IN-1 能透过血脑屏障。
- GC68544 4,5-Dimethoxycanthin-6-one 4,5-Dimethoxycanthin-6-one 是一种有效的、非竞争性的 CYP1A2 介导的 phenacetin O-deethylation 抑制剂,其 IC50 值为 1.7 μM, Ki 值为 2.6 μM。4,5-Dimethoxycanthin-6-one 为生物碱,从 Picrasma quassioides BENNET (Simaroubaceae) 中分离得到。
- GC67933 LKY-047 LKY-047,是 Decursin 的一种衍生物,是一种有效的选择性的可逆竞争性的细胞色素 P45022J2 (CYP2J2) 抑制剂,IC50 为 1.7 μM。LKY-047 对其他人类 P450 无效,例如 CYP1A2、CYP2A6、CYP2B6、CYP2C8、CYP2C9、CYP2C19、CYP2D6、CYP2E1 和 CYP3A。
- GC66197 α-?Terpinyl acetate Terpinyl Acetate (alpha-Terpinyl), a naturally occuring compound found in several essential oils, is a flavouring agent.
- GC52132 N-desmethyl Diltiazem (hydrochloride) An active metabolite of diltiazem
- GC65517 4-(Trifluoromethyl)umbelliferone 4-(Trifluoromethyl)umbelliferone 是大鼠肝细胞色素 P450 酶的荧光探针底物。
- GC65345 BI 653048 BI 653048 是一种选择性且口服的非甾体类糖皮质激素 (glucocorticoid (GC)) 激动剂,其 IC50 值为 55 nM。BI 653048 抑制 CP1A2,CYP2D6,CYP2C9,CYP2C19 和 CYP3A4 的活性并降低对 hERG 离子通道的亲和力 (IC50>30 μM)。BI 653048 源于专利 WO2005028501A1 (化合物 103),它也是一种 HCV NS3 protease 抑制剂,可以减少感染丙型肝炎病毒的病毒载量。
- GC65260 EDP-305 EDP-305 是一种口服有效且选择性的 farnesoid X 受体 (FXR) 激动剂,其 EC50 值为 34 nM (CHO 细胞嵌合性 FXR) 和 8 nM (HEK 细胞全长 FXR)。EDP-305 显示出强大而持久的抗纤维化作用。EDP-305 可用于原发性胆道胆管炎 (PBC) 和非酒精性脂肪性肝炎 (NASH) 研究。
- GC65088 Atovaquone-d5 Atovaquone-d5 (Atavaquone-d5) 是 Atovaquone 的氘代物。Atovaquone (Atavaquone) 是一种有效的、具有口服活性的选择性寄生虫线粒体细胞色素 bc1 (parasite's mitochondrial cytochrome bc1) 复合物的抑制剂。Atovaquone 抑制人类和 P. falciparum 细胞色素 bc1 活性,IC50 值分别为 460 nM 和 2.0 nM。Atovaquone 是一种抗疟 (antimalarial agent) 试剂,有潜力用于肺孢子虫肺炎、弓形体病、疟疾和巴贝斯虫病的相关研究。
- GC52083 21-Deoxycortisone A corticosteroid metabolite of 11-keto progesterone
- GC52062 7-Benzyloxy-4-(trifluoromethyl)coumarin A fluorogenic substrate for CYP1A2 and CYP3A
- GC52060 Trimipramine N-oxide An active metabolite of trimipramine
- GC52045 N-desmethyl Azelastine An active metabolite of azelastine
- GC52038 Desthiazolylmethyl Ritonavir A ritonavir degradation product
- GC52024 Aripiprazole N-oxide A metabolite of aripiprazole
- GC52019 Norpropranolol (hydrochloride) An active metabolite of propranolol
- GC52007 N-hydroxylamine Dapsone An active metabolite of dapsone
- GC49875 (±)-N-desmethyl Venlafaxine (hydrochloride) A minor active metabolite of venlafaxine
- GC49866 Desmethyl Carvedilol An active metabolite of carvedilol
- GC49855 Harmalol (hydrochloride hydrate) A β-carboline alkaloid and an active metabolite of harmaline
- GC49851 Norquetiapine An active metabolite of quetiapine
- GC49842 Digoxigenin Bisdigitoxoside A Na+/K+-ATPase inhibitor
- GC49832 Hydroxymetronidazole An active metabolite of metronidazole
- GC49817 Desethoxy Quetiapine (hydrochloride) An active metabolite of quetiapine
- GC64010 Abiraterone decanoate Abiraterone decanoate 是一种有效的 Abiraterone 前药。Abiraterone decanoate 通过肌肉内 (IM) 递送提供 Abiraterone 的受控释放和长效 CYP17 抑制。
- GC63872 Dagrocorat hydrochloride Dagrocorat (PF-00251802) hydrochloride 是一种具有口服活性,选择性和高亲和性部分糖皮质激素受体的激动剂。Dagrocorat hydrochloride 也是一种时间依赖性可逆抑制剂,对 CYP3A (IC50=1.3 μM) 和CYP2D6 (Ki=0.57 μM) 有抑制作用。Dagrocorat hydrochloride 可用于类风湿性关节炎的研究。
- GC49686 N-desmethyl Regorafenib N-oxide An active metabolite of regorafenib
- GC49629 6β-hydroxy Prednisolone A metabolite of prednisolone
- GC49627 Rabeprazole sulfone A metabolite of rabeprazole
- GC49583 N-desmethyl Sertraline (hydrochloride) A metabolite of sertraline
- GC49559 Hydroxymethyl Tolperisone (hydrochloride) A metabolite of tolperisone
- GC49544 8-hydroxy Mirtazapine A metabolite of mirtazapine
- GC49503 Thujopsene A sesquiterpene with diverse biological activities
- GC49501 Nirvanol An active metabolite of mephenytoin
- GC63469 Abiraterone-D4 Abiraterone-D4 (CB-7598-D4) 是 Abiraterone 的氘代物。Abiraterone 是一种有效的不可逆的 CYP17A1 抑制剂,具有抗雄激素活性,抑制细胞色素 p450 酶 CYP17 的 17α-羟化酶和 17,20-裂合酶活性,IC50 值 分别为 2.5 nM 和 15 nM.
- GC63272 β-Apo-8’-carotenal Apocarotenal is a carotenoid found in spinach and citrus fruits and plays a role as a precursor of vitamin A.
- GC63199 Soticlestat A cholesterol 24-hydroxylase/CYP46A1 inhibitor
- GC49439 (±)11(12)-DiHET MaxSpec® Standard A quantitative analytical standard guaranteed to meet MaxSpec® identity, purity, stability, and concentration specifications
- GC49429 6-keto Lithocholic Acid A metabolite of lithocholic acid
- GC49421 Atorvastatin lactone-d5 An internal standard for the quantification of atorvastatin lactone
- GC49410 CVT-2738 An active metabolite of ranolazine
- GC49409 Desmethyl Ranolazine A metabolite of ranolazine
- GC49403 Benzarone An active metabolite of benzbromarone